ArticleMolecular pharmacology2019
Pharmacological, Mechanistic, and Pharmacokinetic Assessment of Novel Melatonin-Tamoxifen Drug Conjugates as Breast Cancer Drugs.
Open access · bronzeAbstract read
In one paragraph
Article in Molecular pharmacology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
0numbers the graph read from it
0cells of the map it votes in
18citing papers in PubMed
4.7field-weighted citation impact, top 5% of its field
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
18 citing papers in PubMed, 42 citations in OpenAlex.
- Melatonin MT1 Receptor Expression in Luminal Invasive Ductal Breast Carcinoma in Postmenopausal Women.Biomolecules · 2025Article
- Cancer Cells Show Higher Sensitivity to Melatonin-Tamoxifen Drug Conjugates than to Combination of Melatonin and Tamoxifen.ACS omega · 2024Article
- Potential of covalently linked tamoxifen hybrids for cancer treatment: recent update.RSC medicinal chemistry · 2024Review
- Temporal Considerations in Brain Metastases Radiation Therapy: The Intersection of Chronobiology and Patient Profiles.Clocks & sleep · 2024Article
- Loss of keratin 23 enhances growth inhibitory effect of melatonin in gastric cancer.Molecular medicine reports · 2024Article
- Biological action of melatonin on target receptors in breast cancer.Revista da Associacao Medica Brasileira (1992) · 2024Review
- Anticancer Drug Conjugates Incorporating Estrogen Receptor Ligands.Pharmaceutics · 2022Review
- Pro-Apoptotic and Anti-Migration Properties of a Thiazoline-Containing Platinum(II) Complex in MDA-MB-231 Breast Cancer Cells: The Role of Melatonin as a Synergistic Agent.Antioxidants (Basel, Switzerland) · 2022Article
- Melatonin Regulates the Daily Levels of Plasma Amino Acids, Acylcarnitines, Biogenic Amines, Sphingomyelins, and Hexoses in a Xenograft Model of Triple Negative Breast Cancer.International journal of molecular sciences · 2022Article
- Chronoradiobiology of Breast Cancer: The Time Is Now to Link Circadian Rhythm and Radiation Biology.International journal of molecular sciences · 2022Review
- Membrane Melatonin Receptors Activated Cell Signaling in Physiology and Disease.International journal of molecular sciences · 2021Review
- Functional Significance of Selective Expression of ERα and ERβ in Mammary Gland Organ Culture.International journal of molecular sciences · 2021Article
- Dexamethasone and Fumaric Acid Ester Conjugate Synergistically Inhibits Inflammation and NF-κB in Macrophages.Bioconjugate chemistry · 2021Article
- Anti-Inflammatory Activity of Melatonin: a Focus on the Role of NLRP3 Inflammasome.Inflammation · 2021Review
- Towards an Integral Therapeutic Protocol for Breast Cancer Based upon the New HInternational journal of molecular sciences · 2020Review
- A New and Integral Approach to the Etiopathogenesis and Treatment of Breast Cancer Based upon Its Hydrogen Ion Dynamics.International journal of molecular sciences · 2020Review
- Novel Melatonin, Estrogen, and Progesterone Hormone Therapy Demonstrates Anti-Cancer Actions in MCF-7 and MDA-MB-231 Breast Cancer Cells.Breast cancer : basic and clinical research · 2020Article
- Melatonin downregulates TRPC6, impairing store-operated calcium entry in triple-negative breast cancer cells.The Journal of biological chemistryArticle
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
15 authors at 1 institution in 3 countries.
Mahmud HasanDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).ORCID 0000-0003-0192-6166
Mohamed Akmal MarzoukDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Saugat AdhikariDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Thomas D WrightDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Benton P MillerDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Margarite D MatossianDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Steven ElliottDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Maryl WrightDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Madlin AlzoubiDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Bridgette M Collins-BurowDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Matthew E BurowDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Ulrike HolzgrabeDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Darius P ZlotosDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Robert E StratfordDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.).
Paula A Witt-EnderbyDivision of Pharmaceutical, Administrative and Social Sciences, Duquesne University, Pittsburgh, Pennsylvania (M.H., T.D.W., B.P.M., P.A.W.-E.); Department of Pharmaceutical Chemistry, German University in Cairo, New Cairo City, Cairo, Egypt (M.A.M., D.P.Z.); Purdue University, West Lafayette, Indiana (S.A.); Section of Hematology and Medical Oncology, Department of Medicine, Tulane Cancer Center, Tulane University School of Medicine, New Orleans, Louisiana (M.D.M., S.E., M.W., M.A., B.M.C.-B., M.E.B.); Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, Wuerzburg, Germany (U.H.); Indiana University School of Medicine, Indianapolis, Indiana (R.E.S.); and Hillman Cancer Center, University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania (P.A.W.-E.) wittp@duq.edu.ORCID 0000-0002-1844-4457
Tulane University · US
Funding
Kinase mediated suppression of metastasis in breast cancerR01CA174785 · NCI · TULANE UNIVERSITY OF LOUISIANA · PI COLLINS-BUROW, BRIDGETTE MICHELLE · 2016 to 2020
$1.8MNCI NIH HHS R01 CA174785
Abstract
Tamoxifen is used to prevent and treat estrogen receptor-positive (ER+) breast cancer (BC); however, its chronic use can increase uterine cancer risk and induce tamoxifen resistance. Novel melatonin-tamoxifen drug conjugates may be promising to treat BC and may help offset the adverse effects of tamoxifen usage alone due to the presence of melatonin. We synthesized and screened five drug conjugates (C2, C4, C5, C9, and C15 linked) for their effects on BC cell (MCF-7, tamoxifen-resistant MCF-7, mouse mammary carcinoma, MDA-MB-231, and BT-549) viability, migration, and binding affinity to melatonin receptor 1 (MT1R) and estrogen receptor 1 (ESR1). C4 and C5 demonstrated the most favorable pharmacological characteristics with respect to binding profiles (affinity for ESR1 and MT1R) and their potency/efficacy to inhibit BC cell viability and migration in four phenotypically diverse invasive ductal BC cell lines. C4 and C5 were further assessed for their actions against tamoxifen-resistant MCF-7 cells and a patient-derived xenograft triple-negative BC cell line (TU-BcX-4IC) and for their mechanisms of action using selective mitogen-activated protein kinase kinase MEK1/2, MEK5, and phosphoinositide 3-kinase (PI3K) inhibitors. C4 and C5 inhibited tamoxifen-resistant MCF-7 cells with equal potency (IC
Indexed as
AnimalsAntineoplastic AgentsBiological AvailabilityBreast NeoplasmsCell Line, TumorCell MovementCell SurvivalDrug Resistance, NeoplasmEstrogen Receptor alphaFemaleGene Expression Regulation, NeoplasticHumansMAP Kinase Signaling SystemMCF-7 CellsMelatoninMiceAntineoplastic AgentsESR1 protein, humanEstrogen Receptor alphaMelatoninReceptor, Melatonin, MT1Tamoxifen
Identifiers
What OpenQuestion holds
Textmetadata
Read underepoch 390
Registered trials
None linked
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.